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首页 / 抑制剂/激动剂 / 膜转运蛋白 / 钠通道 / Cariporide/卡立泊来德

Cariporide/卡立泊来德 {[allProObj[0].p_purity_real_show]}

货号：A217757 同义名： HOE-642 Free Base; HOE 642

Cariporide是一种选择性Na+/H+交换体异构体1（NHE1）抑制剂，IC50值为0.05 μM，具有心脏保护和抗心律失常作用。

Cariporide/卡立泊来德 化学结构 CAS号：159138-80-4
Cariporide/卡立泊来德 化学结构
CAS号：159138-80-4
Cariporide/卡立泊来德 3D分子结构
CAS号：159138-80-4
Cariporide/卡立泊来德 化学结构 CAS号：159138-80-4
Cariporide/卡立泊来德 3D分子结构 CAS号：159138-80-4
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Cariporide/卡立泊来德 纯度/质量文件 产品仅供科研

货号：A217757 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Sodium Channel ↓ 其他靶点 纯度
Tolperisone HCl ✔ 99%
Triamterene +++

ENaC, IC50: 4.5 μM

 		98%
Lamotrigine ✔ 98%
Vinpocetine ✔ 98%
Zonisamide ✔ 99%
Dronedarone HCl ✔ 95%
Procainamide HCl ✔ 99%
Bupivacaine HCl ✔ 99+%
Benzocaine ✔ 98%
Carbamazepine ++

Sodium channel, IC50: 131 μM

 		98%
Quinidine sulfate dihydrate ✔ 98%
Ibutilide fumarate ✔ 99%+
Dibucaine HCl ✔ 99+%
Mexiletine HCl ✔ 99%
Phenytoin ✔ 99+%
Camostat Mesylate +++

epithelial sodium channel (ENaC), IC50: 50 nM

 		99%+
Levobupivacaine ✔ 97+%
Oxcarbazepine +

sodium channel, IC50: 160 μM

 		98%
Amiloride HCl dihydrate ✔ 97%
Ambroxol 98+%
Primidone ✔ 99%
Propafenone ✔ 99%
A-803467 ++++

Na(V1.8) channel, IC50: 8 nM

 		99%+
Rufinamide ✔ 99%
Phenytoin sodium ✔ 98%
Proparacaine HCl +

Voltage-gated sodium channel, ED50: 3.4 mM

 		98+%
Amiloride HCl ✔ 98%
Riluzole ✔ 97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Cariporide/卡立泊来德 生物活性

描述 Cariporide remarkably suppressed cytosolic Na+ and Ca2+ accumulation. Mitochondrial Ca2+ overload induced by H2O2 was remarkably suppressed by cariporide. Cariporide prevented mitochondrial membrane potential loss induced by H2O2. Cariporide protects cardiomyocytes against oxidant-induced cell death by preserving intracellular ion homeostasis and mitochondrial integrity[3]. Cariporide (HOE-642) ameliorates myocardial ischemia/reperfusion injury, by the well-established reduction of cytosolic Ca2+ in cardiac myocytes through inhibition of Na+/H+ exchange[4]. Cariporide might inhibit HG-mediated monocyte-endothelial cell adhesion and expression of ICAM-1 (intercellular adhesion molecule-1) by inhibiting the activation of NHE-1(Na(+)/H(+) exchanger 1)[5]. Moreover, cariporide significantly facilitates the sensitivity of breast cancer to doxorubicin both in vitro and in vivo[6].

Cariporide/卡立泊来德 细胞实验

Cell Line
Concentration Treated Time Description References
HCT116 cells 1 μM and 10 μM EMPA did not inhibit the activity of the human NHE1 isoform. Cardiovasc Res. 2021 Dec 17;117(14):2794-2806.
rat ventricular cardiomyocytes 10 μM Cariporide nearly completely inhibited NHE1 activity, while EMPA (1, 3, 10, or 30 μM) showed no NHE1 inhibition. Cardiovasc Res. 2021 Dec 17;117(14):2794-2806.
human atrial cardiomyocytes 10 µM 45 min Cariporide significantly reduced Na influx in atrial cardiomyocytes of HFpEF patients. Cardiovasc Res. 2024 Jul 31;120(9):999-1010.
rat ventricular cardiomyocytes 10 μM Cariporide nearly completely inhibited NHE1 activity Cardiovasc Res. 2021 Dec 17;117(14):2794-2806.
cardiomyocytes 10 µM 5 min measure NHE1 activity, Cariporide inhibited NHE1 activity Basic Res Cardiol. 2024 Oct;119(5):751-772.

Cariporide/卡立泊来德 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Rats, mice, and guinea pigs Langendorff-perfused hearts Perfusion 10 μM 15 minutes Cariporide significantly inhibited pH i recovery, while EMPA did not affect [Na+]i or pH i recovery. Cardiovasc Res. 2021 Dec 17;117(14):2794-2806.
Rats Langendorff-perfused hearts Perfusion 10 μM 15 minutes Cariporide significantly inhibited pH recovery and [Na+]i rise Cardiovasc Res. 2021 Dec 17;117(14):2794-2806.
Mice TAC/DOCA-induced heart failure model Oral 600 mg/kg Once daily for 10-12 days Cariporide mimicked EMPA's protection, preventing the development of heart failure Basic Res Cardiol. 2024 Oct;119(5):751-772.
Mice Type 2 diabetic dbb mice Perfusion 1 μM Administered 10 minutes before inducing ischemia and remained throughout the experiment To investigate the role of NHE in cytoplasmic Ca2+ overload and ischemic myocardial damage during ischemia-reperfusion in type 2 diabetic mouse hearts. Results showed that Cariporide significantly reduced Ca2+ overload during ischemia-reperfusion and improved the recovery of ventricular function in diabetic hearts. Cardiovasc Diabetol. 2012 Apr 11;11:33

Cariporide/卡立泊来德 参考文献

[1]Chakrabarti S, Hoque AN, Karmazyn M. A rapid ischemia-induced apoptosis in isolated rat hearts and its attenuation by the sodium-hydrogen exchange inhibitor HOE 642 (cariporide). J Mol Cell Cardiol. 1997 Nov;29(11):3169-74.

[2]Scholz W, Albus U, et al. Protective effects of HOE642, a selective sodium-hydrogen exchange subtype 1 inhibitor, on cardiac ischaemia and reperfusion. Cardiovasc Res. 1995 Feb;29(2):260-8.

[3]Teshima Y, Akao M, Jones SP, Marbán E. Cariporide (HOE642), a selective Na+-H+ exchange inhibitor, inhibits the mitochondrial death pathway. Circulation. 2003 Nov 4;108(18):2275-81

[4]Chang HB, Gao X, Nepomuceno R, Hu S, Sun D. Na(+)/H(+) exchanger in the regulation of platelet activation and paradoxical effects of cariporide. Exp Neurol. 2015 Oct;272:11-6

[5]Wang SX, Sun XY, Zhang XH, Chen SX, Liu YH, Liu LY. Cariporide inhibits high glucose-mediated adhesion of monocyte-endothelial cell and expression of intercellular adhesion molecule-1. Life Sci. 2006 Aug 29;79(14):1399-404

[6]Chen Q, Liu Y, Zhu XL, Feng F, Yang H, Xu W. Increased NHE1 expression is targeted by specific inhibitor cariporide to sensitize resistant breast cancer cells to doxorubicin in vitro and in vivo. BMC Cancer. 2019 Mar 8;19(1):211

Cariporide/卡立泊来德 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.53mL

0.71mL

0.35mL

17.65mL

3.53mL

1.76mL

35.29mL

7.06mL

3.53mL

Cariporide/卡立泊来德 技术信息

CAS号159138-80-4
分子式C12H17N3O3S
分子量 283.35
SMILES Code CS(C1=CC(C(N=C(N)N)=O)=CC=C1C(C)C)(=O)=O
MDL No. MFCD00864683
别名 HOE-642 Free Base; HOE 642
运输蓝冰
InChI Key IWXNYAIICFKCTM-UHFFFAOYSA-N
Pubchem ID 151172
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C
溶解方案

DMSO: 105 mg/mL(370.57 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Cariporide | 159138-80-4 | HOE-642 | HOE642 | HOE 642 | Na+/H+ Exchange Inhibitor | Membrane Transporter/Ion Channel | Na+/H+ Exchanger (NHE) | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Cariporide/卡立泊来德 纯度/质量文件 | Cariporide/卡立泊来德 亚型比较 | Cariporide/卡立泊来德 生物活性 | Cariporide/卡立泊来德 参考文献 | Cariporide/卡立泊来德 实验方案 | Cariporide/卡立泊来德 技术信息

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